B-Raf Selective Inhibitors
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
GDC-0879 is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM with activity against c-Raf as well; no inhibition known to other protein kinases.
|Selective||B-Raf, IC50: 0.13 nM|
SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.
|Selective||B-Raf, Ki: 0.16 nM|
Encorafenib (LGX818) is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing B-RAF(V600E) with EC50 of 4 nM. Phase 3.
|Selective||B-Raf (V600E), EC50: 4 nM|
RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM. Phase 2.
|Selective||B-Raf, IC50: 3 nM-60 nM|
Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively.
|Pan||B-Raf (V600E), IC50: 0.8 nM; B-Raf, IC50: 3.2 nM|
TAK-632 is a potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf, respectively, showing less or no inhibition against other tested kinases.
|Pan||B-Raf, IC50: 8.3 nM|
PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.
|Pan||B-Raf, IC50: 160 nM; B-Raf (V600E), IC50: 13 nM|
CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2.
|Pan||B-Raf (V600E), Kd: 14 nM; B-Raf, Kd: 36 nM|
Sorafenib Tosylate (Bay 43-9006) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.
|Pan||B-Raf (V599E), IC50: 38 nM; B-Raf, IC50: 22 nM|
Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.
|Pan||B-Raf, IC50: 22 nM; B-Raf (V599E), IC50: 38 nM|
|S1267||Vemurafenib (PLX4032, RG7204)||
Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM.
|Pan||B-Raf, IC50: 100 nM; B-Raf (V600E), IC50: 31 nM|
AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc.
|Pan||B-Raf (V600E), IC50: 34 nM; B-Raf, IC50: 105 nM|